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RS-127445

MCE 国际站：RS-127445

品牌：MedChemExpress (MCE)

货号：HY-15419A

CAS 号：199864-87-4

生物活性： RS-127445 是一种选择性高亲和力口服生物利用度高的 5-HT2B 受体拮抗剂，pKi 为 9.5。与许多其他受体和离子通道结合位点相比，RS-127445 对该受体的选择性高出 1000 倍[1]。

体外研究(In Vitro)：RS-127445 is found to has nanomolar affinity for the 5-HT2B receptor (pKi=9.5±0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently displaces [3H]-5-HT from human recombinant 5-HT2B receptors expressed in CHO-K1 cells. The affinity (pKi value) of RS-127445 for the 5-HT2B receptor is 9.5±0.1 (n=9). RS-127445 is selective for the 5-HT2B receptor, having approximately 1000 fold lower affinity for the human recombinant 5-HT2A, 5-HT2C, 5-HT5, 5-HT6 and 5-HT7 receptors, a 5-HT1A receptor in rat brain membranes, a 5-HT1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets. RS-127445 potently blocks the 5-HT (10 nM) evoked increases in intracellular calcium concentrations in the HEK-293 cells expressing the 5-HT2B receptor (pIC50 of 10.4±0.1). In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pKB=9.5±0.1) and 5-HT-evoked increases in intracellular calcium (pIC10=10.4±0.1). RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus (pA2B=9.5±1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2=9.9±0.3)[1]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：In rats, the fraction of RS-127445 that is bioavailable via the oral or intraperitoneal routes is 14 and 60% respectively. Intraperitoneal administration of RS-127445 (5 mg/kg) produced plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4 h.RS-127445 (5 mg/kg) is administered to rats by oral, intraperitoneal and intravenous routes. Peak plasma concentrations are rapidly achieved with the highest concentrations being found at the first time-point measured following intravenous and intraperitonael administration (0.08 h) and by 0.25 h following dosing by the oral route of administration. RS-127445 is cleared from plasma with an estimated terminal elimination half-life of approximately 1.7 h. The bioavailability of RS-127445, when administered by the oral and intraperitoneal routes is approximately 14 and 62% of that obtained by intravenous administration. Approximately 60% of an intraperitoneal dose and 14% of the oral dose of RS-127445 (5 mg/kg) is bioavailable[1]. RS-127445 (1-30 mg/kg), dose-dependently reduces faecal output, reaching significance at 10 and 30 mg/kg (n=6-11). In blood and brain, >98% of RS-127445 is protein-bound[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：281.33

Formula：C17H16FN3

性状：固体

颜色：White to off-white

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式： 4°C，密封保存，避免受潮 *溶剂保存：-80°C，6个月；-20°C，1个月（密封保存，避免受潮）

文献引用：MCE 顾客使用本产品发表 3 篇科研文献

提供质量检测报告：Data Sheet、SDS、COA、LCMS、产品使用指南

产品活性：RS-127445 是一种有效的，具有口服活性的，高亲和力选择性 5-HT2B 受体拮抗剂，pKi 为 9.5，比作用于其他受体和离子通道的选择性高 1000 倍。

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客户发表文献：
[1]. Nature. 2026 Sep;657(8131):549-558.
[2]. Nature. 2026 Sep;657(8132):755-764.
[3]. Nature. 2026 Sep;657(8133):1027-1034.
[4]. Nature. 2026 Sep;657(8131):477-486.
[5].Nature. 2026 Sep;657(8132):789-799.
[6]. Nature. 2026 Sep;657(8131):517-524.
[7]. Nature. 2026 Sep;657(8133):1045-1052.
[8]. Cell. 2026 Sep 14:S0092-8674(26)01003-2.
[9]. Cell. 2026 Sep 3;189(18):5688-5705.e13.
[10]. Cell. 2026 Sep 2:S0092-8674(26)00937-2.

参考文献：
[1]. Bonhaus DW, et al. RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br J Pharmacol. 1999 Jul;127(5):1075-82.